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| - Effects of Side Chain Configuration and Backbone Spacing on theGene Delivery Properties of Lysine-Derived Cationic Polymers
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| - A series of lysine-based oligomers (18 residues) that differ in side chain configuration or side chainspacing along the backbone was tested for DNA transfection activity. Although materials constructedfrom lysine are not the most effective polymeric transfection agents, we have chosen l-lysine-basedmolecules as a starting point because this system allows us to examine the functional effects ofincremental changes in polycation structure. The oligomer constructed from β3-homolysine (β3-hLys)and that from α-d-lysine were superior to an α-l-lysine 18-mer in gene delivery assays. This improvedactivity is attributed to the fact that the α-l-peptide is a protease substrate while the other 18-mersare not. This conclusion is supported by the effects of chloroquine on transfection activity, based onthe protease inhibition activity of chloroquine. To our knowledge, these results represent the firstdirect comparison of a d-lysine oligomer with an l-lysine oligomer in the context of gene delivery.Poly(β3-hLys) was synthesized from the ring opening polymerization of the corresponding lactam. TheDNA transfection ability of this polymer was compared with that of commercially available poly(l-lysine) (PLL). In each case the polymer was more active than the corresponding oligomer.
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